MX2016017395A - Fatty acids and their use in conjugation to biomolecules. - Google Patents

Fatty acids and their use in conjugation to biomolecules.

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Publication number
MX2016017395A
MX2016017395A MX2016017395A MX2016017395A MX2016017395A MX 2016017395 A MX2016017395 A MX 2016017395A MX 2016017395 A MX2016017395 A MX 2016017395A MX 2016017395 A MX2016017395 A MX 2016017395A MX 2016017395 A MX2016017395 A MX 2016017395A
Authority
MX
Mexico
Prior art keywords
disease
conjugate
fatty acid
metabolic disorders
diseases
Prior art date
Application number
MX2016017395A
Other languages
Spanish (es)
Other versions
MX367520B (en
Inventor
Yuan Jun
Yamada Ken
Zecri Frederic
Weninger Barnes David
Marshall Bruce Alexandra
Kanter Aaron
Lou Changgang
Richardson Usera Aimee
Ibebunjo Chikwendu
Duttaroy Alokesh
Clare Kirman Louise
Bose Avirup
Original Assignee
Novartis Ag
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=53491695&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=MX2016017395(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of MX2016017395A publication Critical patent/MX2016017395A/en
Publication of MX367520B publication Critical patent/MX367520B/en

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    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
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    • C12N15/00—Mutation or genetic engineering; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification; Use of hosts therefor
    • C12N15/09—Recombinant DNA-technology
    • C12N15/11—DNA or RNA fragments; Modified forms thereof; Non-coding nucleic acids having a biological activity
    • C12N15/113—Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides; Antisense DNA or RNA; Triplex- forming oligonucleotides; Catalytic nucleic acids, e.g. ribozymes; Nucleic acids used in co-suppression or gene silencing
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    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/543—Lipids, e.g. triglycerides; Polyamines, e.g. spermine or spermidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/08—Peptides having 5 to 11 amino acids
    • A61K38/095—Oxytocins; Vasopressins; Related peptides
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/164—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from bacteria
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/1703—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates
    • A61K38/1709—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates from mammals
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/18—Growth factors; Growth regulators
    • A61K38/1825—Fibroblast growth factor [FGF]
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    • A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/18—Growth factors; Growth regulators
    • A61K38/1841—Transforming growth factor [TGF]
    • A—HUMAN NECESSITIES
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    • A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/22—Hormones
    • A61K38/2221—Relaxins
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
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    • A61K47/542—Carboxylic acids, e.g. a fatty acid or an amino acid
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    • A61P3/06—Antihyperlipidemics
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    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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    • A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
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    • A61P5/50—Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
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    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C55/00—Saturated compounds having more than one carboxyl group bound to acyclic carbon atoms
    • C07C55/02—Dicarboxylic acids
    • C—CHEMISTRY; METALLURGY
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    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C55/00—Saturated compounds having more than one carboxyl group bound to acyclic carbon atoms
    • C07C55/22—Tricarboxylic acids
    • C—CHEMISTRY; METALLURGY
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    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C57/00—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms
    • C07C57/02—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms with only carbon-to-carbon double bonds as unsaturation
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    • C07C57/02—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms with only carbon-to-carbon double bonds as unsaturation
    • C07C57/13—Dicarboxylic acids
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    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C59/00—Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C59/235—Saturated compounds containing more than one carboxyl group
    • C07C59/245—Saturated compounds containing more than one carboxyl group containing hydroxy or O-metal groups
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    • C07C59/235—Saturated compounds containing more than one carboxyl group
    • C07C59/245—Saturated compounds containing more than one carboxyl group containing hydroxy or O-metal groups
    • C07C59/285—Polyhydroxy dicarboxylic acids having five or more carbon atoms, e.g. saccharic acids
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    • C12N2310/00—Structure or type of the nucleic acid
    • C12N2310/10—Type of nucleic acid
    • C12N2310/14—Type of nucleic acid interfering N.A.
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    • C12N2310/00—Structure or type of the nucleic acid
    • C12N2310/30—Chemical structure
    • C12N2310/35—Nature of the modification
    • C12N2310/351—Conjugate

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Immunology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Zoology (AREA)
  • Diabetes (AREA)
  • Genetics & Genomics (AREA)
  • Biomedical Technology (AREA)
  • Cardiology (AREA)
  • Molecular Biology (AREA)
  • Endocrinology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Biotechnology (AREA)
  • General Engineering & Computer Science (AREA)
  • Wood Science & Technology (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Biophysics (AREA)
  • Plant Pathology (AREA)
  • Marine Sciences & Fisheries (AREA)
  • Biochemistry (AREA)
  • Microbiology (AREA)
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  • Vascular Medicine (AREA)
  • Hospice & Palliative Care (AREA)

Abstract

The invention provides a conjugate comprising a biomolecule linked to a fatty acid via a linker wherein the fatty acid has the following Formulae A1, A2 or A3: wherein R1, R2, R3, R4, Ak, n, m and p are defined herein. The invention also relates to a method for manufacturing the conjugate of the invention such as GDF15 conjugate, and its therapeutic uses such as treatment or prevention of metabolic disorders or diseases, type 2 diabetes mellitus, obesity, pancreatitis, dyslipidemia, alcoholic and nonalcoholic fatty liver disease/steatohepatitis and other progressive liver diseases, insulin resistance, hyperinsulinemia, glucose intolerance, hyperglycemia, metabolic syndrome, hypertension, cardiovascular disease, atherosclerosis, peripheral arterial disease, stroke, heart failure, coronary heart disease, diabetic complications (including but not limited to chronic kidney disease), neuropathy, gastroparesis and other metabolic disorders. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
MX2016017395A 2014-06-23 2015-06-18 Fatty acids and their use in conjugation to biomolecules. MX367520B (en)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201462015862P 2014-06-23 2014-06-23
US201462082327P 2014-11-20 2014-11-20
US201562107016P 2015-01-23 2015-01-23
PCT/US2015/036328 WO2015200078A1 (en) 2014-06-23 2015-06-18 Fatty acids and their use in conjugation to biomolecules

Publications (2)

Publication Number Publication Date
MX2016017395A true MX2016017395A (en) 2017-05-01
MX367520B MX367520B (en) 2019-08-26

Family

ID=53491695

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2016017395A MX367520B (en) 2014-06-23 2015-06-18 Fatty acids and their use in conjugation to biomolecules.

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US (4) US10588980B2 (en)
EP (2) EP3157571B1 (en)
JP (5) JP6636959B2 (en)
KR (2) KR20230056796A (en)
CN (3) CN114133443A (en)
AP (1) AP2016009585A0 (en)
AU (1) AU2015280351C1 (en)
CA (1) CA2953480A1 (en)
CL (1) CL2016003281A1 (en)
CR (1) CR20160596A (en)
CU (1) CU24455B1 (en)
CY (1) CY1125006T1 (en)
DK (1) DK3157571T3 (en)
EA (1) EA039074B1 (en)
EC (1) ECSP17004665A (en)
ES (1) ES2905479T3 (en)
GT (1) GT201600263A (en)
HK (1) HK1232160A1 (en)
HR (1) HRP20220152T1 (en)
HU (1) HUE057845T2 (en)
IL (1) IL248990B (en)
JO (1) JO3813B1 (en)
LT (1) LT3157571T (en)
MA (1) MA40278A (en)
MX (1) MX367520B (en)
MY (1) MY193993A (en)
PE (1) PE20171095A1 (en)
PH (1) PH12016502294B1 (en)
PL (1) PL3157571T3 (en)
PT (1) PT3157571T (en)
RS (1) RS62907B1 (en)
SG (2) SG10201912965TA (en)
SI (1) SI3157571T1 (en)
TN (1) TN2016000558A1 (en)
TW (3) TWI750725B (en)
UY (1) UY36186A (en)
WO (1) WO2015200078A1 (en)

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US8420088B2 (en) 2008-01-28 2013-04-16 Novartis Ag Methods and compositions using FGF23 fusion polypeptides
TW200936156A (en) 2008-01-28 2009-09-01 Novartis Ag Methods and compositions using Klotho-FGF fusion polypeptides
AU2012240102C1 (en) 2011-04-08 2016-09-08 Amgen Inc. Method of treating or ameliorating metabolic disorders using growth differentiation factor 15 (GDF-15)
BR112016002213A2 (en) 2013-07-31 2017-08-29 Amgen Inc CONSTRUCTS OF GROWTH DIFFERENTIATION FACTOR 15 (GDF-15)
US10588980B2 (en) 2014-06-23 2020-03-17 Novartis Ag Fatty acids and their use in conjugation to biomolecules
EA201791238A1 (en) 2014-12-04 2018-02-28 Новартис Аг METHODS AND COMPOSITIONS IN WHICH OPTIONS OF KLOTHO POLYPEPTIDES ARE USED
MA41580A (en) 2015-01-23 2017-11-29 Novartis Ag SYNTHETIC APELIN FATTY ACID CONJUGATES WITH IMPROVED HALF-LIFE
US10633653B2 (en) 2015-08-14 2020-04-28 University Of Massachusetts Bioactive conjugates for oligonucleotide delivery
CN108367053A (en) * 2015-12-22 2018-08-03 诺华股份有限公司 The method that metabolic disease is treated or improved using growth and differentiation factor 15 (GDF-15)
EP3408391A4 (en) 2016-01-31 2019-08-28 University of Massachusetts Branched oligonucleotides
JP7013390B2 (en) 2016-05-24 2022-01-31 ノヴォ ノルディスク アー／エス MIC-1 compound and its use
KR101727506B1 (en) * 2016-07-14 2017-05-04 충남대학교 산학협력단 Pharmaceutical composition for the prevention or treatment of fat liver comprising GDF15 protein or polynucleotide encoding GDF15 as an effective ingredient
CA3033368A1 (en) * 2016-08-12 2018-02-15 University Of Massachusetts Conjugated oligonucleotides
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